| Pharmacodynamic actions of midodrine, a new alpha-adrenergic stimulating agent, and its main metabolite, ST 1059. | |
| | |
MedLine Citation:
|
PMID: 66056 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
Pharmacodynamic actions of alpha-(2,5-dimethoxyphenyl)-beta-glycinamido-ethanol-hydrochloride (midodrine, Gutron) and alpha-(2,5-dimethoxy-phenyl)-beta-aminoethanol (ST 1059), the main metabolite of midodrine, were investigated in various experimental procedures. Midodrine raises arterial blood pressure both after parenteral and enteral administration in animal experiments. Midodrine increases peripheral vascular tone when given in doses still ineffective in raising blood pressure. The d(+)-isomer of midodrine is by far less effective than the racemic mixture. Pretreatment with atropine, reserpine, guanethidine or hexamethonium has no influence on midodrine activity. Midodrine effects are greatly reduced by phentolamine but rather enhanced by propranolol pretreatment. Midodrine raises blood pressure in pithed rats, too; in the experiments performed the drug is devoid of central effects even when high doses are given. Chronic pretreatment with midodrine over a longer period reduces the effect of a subsequent single injection of this substance. Because of the results cited above midodrine may be classified as a direct peripheral alpha-adrenergic stimulating agent. alpha-Adrenergic receptor stimulation induced by midodrine can be demonstrated in various smooth muscle organs (blood vessels, nictitating membrane, intestine, pupil, urinary bladder, bronchi). In contrast to other pressor sympathomimetic agents, midodrine is of long duration of action and good efficacy after enteral administration. ST 1059, the main metabolite of midodrine, is an active alpha-adrenergic stimulating agent with a shorter duration of action than midodrine. It is suggested that midodrine is the well-absorbed "transport form", from which ST 1059, the actural pressor agent, is formed enzymatically in organism. |
| | |
Authors:
|
H Pittner; H Stormann; R Enzenhofer |
Related Documents
:
|
239806 - Normal cardiac output during beta blockade with timolol in hypertensive patients. 2572366 - Acute changes in the properties of baroreflexes in man after beta-blockade. 7870896 - Beta-receptor responsiveness after desipramine treatment. 6199596 - Beta-adrenoceptor selectivity of dobutamine: in vivo and in vitro studies. 9301396 - Effects of alfentanil on cerebral haemodynamics in an experimental model of traumatic b... 2410726 - Role of vascular alpha 2-adrenoceptors as targets for circulating catecholamines in the... |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Arzneimittel-Forschung Volume: 26 ISSN: 0004-4172 ISO Abbreviation: Arzneimittelforschung Publication Date: 1976 |
Date Detail:
|
Created Date: 1977-04-28 Completed Date: 1977-04-28 Revised Date: 2007-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 0372660 Medline TA: Arzneimittelforschung Country: GERMANY, WEST |
Other Details:
|
Languages: eng Pagination: 2145-54 Citation Subset: IM |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Adrenergic alpha-Agonists* Animals Blood Pressure / drug effects Capillary Permeability / drug effects Cats Decerebrate State Dogs Ethanolamines / pharmacology* Female Guinea Pigs Hemodynamics / drug effects Hypotension / drug therapy Male Mice Midodrine / metabolism, pharmacology* Muscle, Smooth / drug effects Rabbits Rats Vasomotor System / drug effects |
| Chemical | |
Reg. No./Substance:
|
0/Adrenergic alpha-Agonists; 0/Ethanolamines; 42794-76-3/Midodrine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: "Physiological interaction" does not explain the H-2 requirement for recognition of virus-infected c...
Next Document: Immunogenicity of macrophage RNA and its properties.